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Unlocking Transformative Cancer Therapies

The Exelixis pipeline includes our lead compounds, cabozantinib and cobimetinib, as well as other programs that are the subject of partnerships and collaborations with several biopharmaceutical companies. An additional wholly owned compound, XL888, is the subject of ongoing clinical research through our Investigator-Sponsored Trial program. Safety and efficacy for these compounds in the unapproved uses or indications described below have not yet been established.

Pipeline Overview

Cabozantinib

Exelixis focuses its internal development efforts primarily upon cabozantinib, a targeted agent that inhibits the activity of receptor tyrosine kinases including MET, AXL, VEGF Receptors, and RET. These receptor tyrosine kinases are involved in both normal cellular function and in pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, and maintenance of the tumor microenvironment. Exelixis discovered cabozantinib internally and maintains exclusive rights to commercialize the product in the United States. Outside of the United States, Ipsen has exclusive commercialization and development rights for current and future cabozantinib indications, except in Japan, where Exelixis has granted exclusive rights to Takeda. Exelixis and its partners are collaborating on the global development plan for cabozantinib and Ipsen and Takeda are responsible for the development work supporting cabozantinib in their respective regions.

Cobimetinib

Cobimetinib, an Exelixis-discovered compound, is a reversible inhibitor of MEK, part of the RAS/RAF/MEK/ERK pathway that is frequently dysregulated in human tumors. Cobimetinib is being developed by Genentech, a member of the Roche Group, under a collaboration agreement with Exelixis and is the subject of a broad clinical development program in combination with a variety of investigational and approved therapies.

Cobimetinib is now approved in multiple countries, including the United States, European Union, Switzerland, Canada, Australia and Brazil, to treat specific forms of BRAF mutation-positive unresectable or metastatic melanoma, in combination with vemurafenib. The trade name for cobimetinib is COTELLIC®. For more information on COTELLIC, including important safety information, please click here.

XL888

XL888 is a highly potent, orally bioavailable ATP-competitive inhibitor of HSP90, a molecular chaperone protein that affects the activity and stability of a range of key regulatory proteins, including kinases such as BRAF, MET, and VEGFR2. Exelixis discovered XL888 and owns the compound exclusively.